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Related Experiment Videos

Substrate specificity of bleomycin hydrolase.

S M Sebti1, J C DeLeon, L T Ma

  • 1Department of Pharmacology, Yale University, School of Medicine, New Haven, CT 06510.

Biochemical Pharmacology
|January 1, 1989
PubMed
Summary
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Bleomycin hydrolase metabolizes various bleomycin analogs, reducing their cancer cell toxicity. Structural changes impact enzyme kinetics, revealing substrate specificity for this protective enzyme.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Enzymology

Background:

  • Bleomycin (BLM) hydrolase protects tissues from the antitumor drug BLM.
  • The substrate specificity of BLM hydrolase is not well understood.

Purpose of the Study:

  • To investigate the substrate specificity of BLM hydrolase.
  • To characterize the metabolism of various BLM analogs by BLM hydrolase.

Main Methods:

  • Developed ion-paired reverse-phase high-speed liquid chromatography systems.
  • Assayed the metabolism of several BLM analogs using rabbit lung BLM hydrolase.

Main Results:

  • BLM hydrolase metabolized BLM A2, BLM B2, tallysomycin S10b, peplomycin, BAPP, deglyco BLM A2, and bleomycinic acid into single metabolites.

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  • Metabolites showed 6- to 35-fold less potency in inhibiting cancer cell proliferation.
  • Kinetic analysis revealed that terminal amine substitutions affected Km, while carbohydrate group deletion influenced Vmax.

    • Conclusions:

    • BLM hydrolase recognizes and metabolizes a broad range of BLM analogs.
    • Metabolism by BLM hydrolase inactivates BLM analogs, reducing their cytotoxicity.
    • Terminal amine and carbohydrate regions dictate substrate affinity and metabolism rate, respectively.